Formulation of oxypurinol and/or its alkali and alkaline earth salts

Abstract

Formulations of oxypurinol and/or its alkali or alkaline earth salts in non-crystalline form, containing the active substance in the form of a solids dispersion with pharmacologically harmless adjuvants. They have more rapid and higher solubility than oxypurinol and/or its alkali or alkaline earth salts. They can be used for the preparation of drugs having high bioavailability of the active substance oxypurinol.

We claim: 
     
       1. Formulation of oxypurinol or its alkali or alkaline earth salt in non-crystalline form, wherein the oxypurinol or its salt is contained in the form of a solids dispersion with pharmacologically inert adjuvants in a ratio of from 1:0.2 to 1:10. 
     
     
       2. A formulation according to claim 1, wherein the ratio of oxypurinol or its salt to adjuvants is from 1:1 to 1:4. 
     
     
       3. A formulation according to claim 1, wherein oxypurinol contained therein has a rate of dissolution of more than 100 mg/l per 5 minutes at a pH range of between 1.0 and 7.5. 
     
     
       4. A formulation according to claim 1, which contains additional active substances. 
     
     
       5. A process for the preparation of a formulation of oxypurinol or its alkali or alkaline earth salts in non-crystalline form, wherein the oxypurinol or its salt and pharmacologically inert adjuvants, at a ratio of 1:0.2 to 1:10, are dissolved together in a solvent or melted together, and then cooled and/or dried, avoiding crystallization. 
     
     
       6. The process as claimed in claim 5, wherein the ratio of oxypurinol or its salt to adjuvants is 1:1 to 1:4. 
     
     
       7. The process as claimed in claim 5, wherein water is used as a solvent. 
     
     
       8. A method of treating hyperuricaemia and gout, comprising administering to a patient in need thereof a formulation according to claim 1. 
     
     
       9. A formulation according to claim 1, wherein the non-crystalline form of oxypurinol maintains a solubility greater than its constant saturation concentration for more than one hour. 
     
     
       10. A formulation according to claim 2, wherein the non-crystalline form of oxypurinol maintains a solubility greater than its constant saturation concentration for more than one hour.